Synonyms: trans‐4‐butylcyclohexane carboxylic acid
Compound class:
Synthetic organic
Comment: X-ray crystallography shows that 4‐BCCA inhibits AMPA receptor activity by binding (with low‐affinity) to a region in the receptor's transmembrane domain (PDB ID 6XSR) [1]. The interaction was confirmed by mutagenesis of the amino acids predicted to be involved in the ligand-receptor interaction by the X-ray structure and electropysiological measurements in vitro. This discovery helps to explain the molecular mechanism underlying 4‐BCCA's anti-epileptic activity.
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Bioactivity Comments |
Wild‐type GluA2 receptors (a subunit of functional AMPA receptors) expressed in HEK293 cells are weakly inhibited by 4‐BCCA: 2 nM inhibits channel current by 40% by electrophysiology [1]. |
Selectivity at ion channels | ||||||||||||||||||||||||||||||||||
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